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Boron containing DOAI

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514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

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DocumentTitleDate
20130045949ANTI-CANCER AGENTS - Described herein are compounds that may be selectively activated to produce active anti-cancer agents in tumor cells. Also disclosed are pharmaceutical compositions comprising the compounds, and methods of treating cancer using the compounds.02-21-2013
20110201574FATTY ACID AMIDE HYDROLASE INHIBITORS - The present invention provides fatty acid amide hydrolase inhibitors, solid forms thereof, compositions thereof, and methods of making and using the same.08-18-2011
20080261921FUSED RING HETEROCYCLE KINASE MODULATORS - The present invention provides fused ring heterocycles as kinase modulators, pharmaceutical compositions containing these modulators, and methods of using these modulators to treat diseases mediated by kinase activity.10-23-2008
20110195931METHODS AND COMPOSITIONS FOR REDUCING NEURONAL CELL DEATH - Methods and compositions involving a class of boron-protected phenylphosphine agents having increased cell permeability and having improved chemical stability for treating or for preventing neuronal cell death-related diseases or conditions in a human or a non-human animal.08-11-2011
20100081632High-content and high throughput assays for identification of lipid-regulating pathways, and novel therapeutic agents for lipid disorders - A method of assaying protein-protein interactions associated with proteins involved in lipid pathways using a protein fragment complementation assays, said method comprising the steps of: (a) identifying protein molecules that interact with said protein associated with lipid pathways; (b) selecting a protein reporter molecule; (c) effecting fragmentation of said protein reporter molecule such that said fragmentation results in reversible loss of reporter function; (d) fusing or attaching fragments of said protein reporter molecule separately to said interacting protein molecules as defined in step (a); (e) transfecting cells with nucleic acid constructs coding for the products of step (d); (f) reassociating said reporter fragments through interactions of the protein molecules that are fused or attached to said fragments; and (g) measuring directly or Indirectly the activity of said reporter molecule resulting from the reassociation of said reporter fragments.04-01-2010
20090018104Triarylcarboxylic Acid Derivative - Provided is a triarylcarboxylic acid derivative, or an isomer, a prodrug, a hydrate, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof, represented by the following general formula (I):01-15-2009
20100113392METHODS OF USING SAHA AND BORTEZOMIB FOR TREATING MULTIPLE MYELOMA - The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor such as suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of one or more anti-cancer agents, including Bortezomib. The HDAC inhibitor and the anti-cancer agent may be administered to comprise therapeutically effective amounts. In various aspects, the effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.05-06-2010
20100075925Hyperthermic Technologies And Therapeutic Uses Thereof - The present invention provides nanoscale and microscale compositions useful for a variety of purposes, including the diagnosis and treatment of diseases. In one embodiment, the present invention provides a disease treatment system comprising a thermal induction agent and a radiation source, wherein the thermal induction agent comprises at least one carbon nanotube, at least one carbon microtube, or a mixture thereof.03-25-2010
20130079303Inhibitors of PI3 Kinase and/or mTOR - The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof;03-28-2013
20130079304Pharmaceutical Compositions for the Treatment of Fungal Infections - Synergistic combinations of a squalene epoxidase inhibitor and a leucyl-tRNA synthetase inhibitor are provided, which are useful in particular in the treatment of diseases involving fungal or suspected fungal infection, for immunomodulation or immunosuppression in conditions in which fungal or suspected fungal colonisation of e.g. the skin or nail plays a role, such as atopic dermatitis, acne vulgaris, seborrhoeic dermatitis, rosacea or onychomycosis, and in situations of fungal resistance.03-28-2013
20130035312CATHEPSIN CYSTEINE PROTEASE INHIBIORS - This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.02-07-2013
20130035311PROCHELATORS FOR INHIBITING METAL-PROMOTED OXIDATIVE STRESS - The present invention provides compounds of Formula I along with compositions containing the same and methods of use thereof in treating oxidative stress.02-07-2013
201300793053-SUBSTITUTED VINYLBORONATES AND USES THEREOF - 3-substituted vinylboronates and their use in the treatment of cancer such as colorectal cancer are disclosed. In some embodiments, the 3-substituted vinylboronates have the general Formula I:03-28-2013
20130079306HETEROCYCLIC COMPOUND AND p27Kip1 DEGRADATION INHIBITOR - A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p2703-28-2013
20130040912PIPERAZINOTRIAZINES AS PI3K INHIBITORS FOR USE IN THE TREATMENT ANTIPROLIFERATIVE DISORDERS - The invention relates to compounds of formula (I) R1 is methyl, n-hexyl, aminoethyl, methylaminoethyl, ethylaminoethyl, dimethylaminoethyl, acryloylaminoethyl, methacryloylaminoethyl, methoxyethyl, ethoxyethyl, d-C4-alkyl-sulfonyl, acryloyl, or methacryloyl; or R1 is aminoethyl, acryloyl or acryloylaminoethyl carrying a linker and a tag, and R2 and R3, independently of each other, are hydrogen or CrC4-alkyl, or R2 and R3 together form a methylene or an ethylene bridge; and tautomers, solvates and pharmaceutically acceptable salts thereof. These compounds are effective in preventing or treating a disease or disorder modulated by PI3 kinases and/or mTOR, in particular treating a hyperproliferative disorder.02-14-2013
20100041628NOVEL INDOLE DERIVATIVE HAVING IKAPPAB KINASE BETA INHIBITORY ACTIVITY - Disclosed is a compound represented by the general formula (1) or a salt thereof. The compound or a salt thereof has an inhibitory activity on IKKβ and is therefore useful as preventive and/or therapeutic agent for a disease associated with IKKβ. In the formula, R02-18-2010
20090124578SPIRO-OXAZOLIDINONE COMPOUNDS AND THEIR USE AS METABOTROPIC GLUTAMATE RECEPTOR POTENTIATORS - Compounds in accord with Formula I:05-14-2009
20100081633Derivatives of 1-amino-2-cyclobutylethylboronic acid - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.04-01-2010
20130090309AMINO-PYRIDINE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS - The invention provides certain amino-pyridine-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R04-11-2013
20100137247Anti-inflammatory compositions and methods - Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.06-03-2010
20130059819INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III).03-07-2013
20120225846HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK - Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.09-06-2012
20120115813BORON-CONTAINING SMALL MOLECULES - This invention relates to, among other items, benzoxaborole compounds and their use for treating bacterial infections.05-10-2012
20090012044Novel Hiv Protease Inhibitors - The present invention provides novel HIV protease inhibitors containing substituted borane, carborane or metallacarborane clusters with 6 to 12 boron atoms in each cluster. The charge of each borane, carborane or metallacarborane cluster is 0, −1 or −2. The number of borane, carborane or metallacarborane clusters in the inhibitor molecule is 1 to 9, and the carborane clusters in metallacarborane inhibitors are coordinated to transition metal atom, selected from the group containing cobalt, iron, nickel and ruthenium. In the cluster, heteroatoms can be present, such as nitrogen, phosphorus, silicon, germanium, tin and sulphur. The present invention covers pharmaceutical compositions containing these inhibitors and their use, both in vitro and in vivo. They are characterized by high effectiveness and stability.01-08-2009
20100087396Novel Compounds Having Selective Inhibiting Effect at GSK3 - The present invention relates to new compounds of formula I04-08-2010
20130165411TRICYCLIC BORON COMPOUNDS FOR ANTIMICROBIAL THERAPY - Provided herein are antimicrobial tricyclic boron compounds of the following formula I:06-27-2013
20090124577Intermediate Compounds for the Preparation of an Angiotensin II Receptor Antagonist - It comprises new substituted 4-valinylmethylphenyl boronic acids of formula (II) and their derivatives and also its preparation process. It also comprises a preparation process of Valsartan (I) from such intermediates. The process comprises the reaction of the new 4-valinylmethylphenyl boronic compounds with a (halophenyl)tetrazole compound which proceeds with high yields. The process is particularly advantageous in its practical industrial realization because it avoids the use of azide derivatives and also the use of expensive biphenyl intermediates.05-14-2009
20100069331TREATMENT OR PREVENTION OF CANCER AND PRECANCEROUS DISORDERS - The NSAID, sulindac and/or its metabolites and derivatives, in combination with an agent that generates or induces reactive oxygen species (ROS), significantly enhances the killing of abnormal cells but does not affect normal cells. This effect occurs at concentrations of each compound that individually have little or no activity directed against the abnormal cells.03-18-2010
20100137249COMPOSITIONS FOR REGULATING OR MODULATING QUORUM SENSING IN BACTERIA, METHODS OF USING THE COMPOUNDS, AND METHODS OF REGULATING OR MODULATING QUORUM SENSING IN BACTERIA - The present disclosure encompasses compounds and compositions that are useful as specific AI-2 antagonists for the control of bacterial quorum sensing. Although the AI-2 antagonists according to the present disclosure may not have bactericidal effect, their ability to attenuate virulence, drug resistance, and/or biofilm formation have therapeutic benefits. In addition, the AI-2 antagonists of the present disclosure can also be used as tools to probe bacterial AI-2 functions. The present disclosure also encompasses methods for inhibiting or attenuating microbial virulence, biofilm formation, and drug resistance. The methods are suitable for preventing bacteria from accruing and forming extensive biofilms that may be a health or hygiene hazard or a physical issue, such as in the blockage of water or fuel lines.06-03-2010
20100144673Diagnosis, prognosis and identification of potential therapeutic targets of multiple myeloma based on gene expression profiling - Gene expression profiling is a powerful tool that has varied utility. It enables classification of multiple myeloma into subtypes and identifying genes directly involved in disease pathogensis and clinical manifestation. The present invention used gene expression profiling in large uniformly treated population of patients with myeloma to identify genes associated with poor prognosis. It also demonstrated that over-expression of CKS1B gene, mainly due to gene amplification that was determined by Fluorescent in-situ hybridization to impart a poor prognosis in multiple myleoma. It is further contemplated that therapeutic strategies that directly target CKS1B or related pathways may represent novel, and more specific means of treating high risk myeloma and may prevent its secondary evolution.06-10-2010
20090325903BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.12-31-2009
20110301124PROTEASOME INHIBITORS - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.12-08-2011
20110288052NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, AND METHODS OF USE FOR SAME - The class compounds of the present invention may be represented by Formula (I), wherein X may be O, S, or N. R11-24-2011
20110021461COMBINATIONS TO IMPROVE ANIMAL HEALTH AND PERFORMANCE - The present invention provides combinations of dietary supplements and methods of using of these combinations to improve the health and production performance of animals. In particular, the combinations of the invention comprise antioxidants, trace minerals, organic acids, essential amino acids, and mixtures thereof.01-27-2011
20110263530Aurora Kinase Modulators and Method of Use - The present invention relates to chemical compounds having a general formula I10-27-2011
20090069271WOOD TREATMENT - A method of introducing boron as a boron ester into timber via a non-aqueous liquid medium. The borate ester may have the formula I: (R03-12-2009
20100267671COMPOSITIONS AND METHODS FOR APOPTOSIS MODULATORS - The present invention includes and relates generally to compounds which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.10-21-2010
20090042836Proteasome inhibitors - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.02-12-2009
20120190646Compositions Comprising Thalidomide and Artemisinin for the Treatment of Cancer - The present invention relates to pharmaceutical compositions for the treatment of cancer and especially for the treatment of hematological malignancies such as multiple myeloma. Specifically, the present invention relates to pharmaceutical composition for the treatment of cancer comprising: thalidomide, or a derivative thereof, or salts or solvates thereof; one or more artemisinin compounds, or salts or solvates thereof; and one or more pharmaceutically acceptable carriers and/or excipients.07-26-2012
20100120716MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS AND USES THEREFOR - Macrocyclic inhibitors of Hepatitis C protease are provided, the inhibitors including a boronic acid or ester group, a macrocyclic ring of about 13 to 25 atoms including at least two amide linkages, a proline-analogous group, and a connecting segment joining moieties on either side of the proline-analogous group. Methods of making the HCV protease-inhibitory compounds, methods of using the compounds, formulations of the compounds, and pharmaceutical combinations including the compounds, are provided.05-13-2010
20100120715BETA-LACTAMASE INHIBITORS - Disclosed herein are α-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising α-aminoboronic acids and methods of use thereof.05-13-2010
20090221527TUMOR NECROSIS FACTOR INHIBITORS - The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-α mediated conditions.09-03-2009
20120295875BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS - This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.11-22-2012
20110172186INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provides compounds, and pharmaceutically acceptable compositions thereof, encompassed by any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof. The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof.07-14-2011
20100249066METHODS OF MODULATING INFLAMMATORY CELL RECRUITMENT AND GENE EXPRESSION USING HALOARYL SUBSTITUTED AMINOPURINES - Provided herein are Aminopurine Compounds having the following structure:09-30-2010
20120035133Lyophilization Cakes of Proteasome Inhibitors - Lyophilized cakes of proteasome inhibitors are described, as well as methods for their production and use.02-09-2012
20090291918PROTEASOME INHIBITORS AND METHODS OF USING THE SAME - The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.11-26-2009
20110172188USE OF ANTI-CONNEXIN AGENTS FOR MODULATING THE THERAPEUTIC EFFECT OF PSYCHOTROPIC DRUGS - The invention first relates to a product containing at least one connexin-blocking agent and a psychotropic drug as combination products for use simultaneously, separately, or spread over time in patients suffering from psychiatric and/or neurodegenerative disorders. The connexin-blocking agent is advantageously selected from the group comprising meclofenamic acid, 18-β-glycyrrhetinic acid, carbenoxolone, mefloquine, and 2-APB, and preferably consists of meclofenamic acid. The invention first relates to a product containing at least one connexin-blocking agent and a psychotropic drug as combination products for use simultaneously, separately, or spread over time in patients suffering from psychiatric and/or neurodegenerative disorders. The connexin-blocking agent is advantageously selected from the group comprising meclofenamic acid, 18-β-glycyrrhetinic acid, carbenoxolone, mefloquine, and 2-APB, and preferably consists of meclofenamic acid.07-14-2011
20110172189Aryl-Phenyl-Sulfonamido-Cycloalkyl Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumour, etc. Formula (I).07-14-2011
20110172187BORON-CONTAINING SMALL MOLECULES - This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections.07-14-2011
20110269715ABNORMAL CANNABIDIOLS AS AGENTS FOR LOWERING INTRAOCULAR PRESSURE - The present invention provides a method of treating glaucoma or ocular hypertension which comprises applying to the eye of a person in need thereof an amount sufficient to treat glaucoma or ocular hypertension of a compound of formula I11-03-2011
20100298268CONTROLLED RELEASE FORMULATIONS OF LEVODOPA AND USES THEREOF - The current invention provides a controlled release oral solid formulation of levodopa comprising levodopa, a decarboxylase inhibitor, and a carboxylic acid. Also provided by this invention is multiparticulate, controlled release oral solid formulations of levodopa comprising: i) a controlled release component comprising a mixture of levodopa, a decarboxylase inhibitor and a rate controlling excipient; ii) a carboxylic acid component; and iii) an immediate release component comprising a mixture of levodopa and a decarboxylase inhibitor.11-25-2010
20120295874COFERONS AND METHODS OF MAKING AND USING THEM - The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 μM and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore.11-22-2012
20080280856Fibroblast Activation Protein Inhibitor Compounds and Methods - Amino terminus-blocked peptide boronate compounds of Formulas I and II are useful for inhibiting Fibroblast Activation Protein (FAP) and other proteases, and for treating disorders mediated by FAP. Methods of using the amino terminus blocked peptide boronate compounds, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.11-13-2008
20080221068ANTI-TUMOR AGENTS - A method for treating subjects with abnormal cell proliferation is provided. The method involves administering to subjects in need of such treatment an effective amount of an agent of Formula I, to inhibit cell proliferation such as that associated with tumor growth and metastasis. A method for inhibiting angiogenesis in an abnormal proliferative cell mass by the administration of an agent of Formula I is also provided.09-11-2008
20090005344Compounds and Methods of Use Thereof - Imidazole and benzimidazole boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof.01-01-2009
20100137246Anti-inflammatory compositions and methods - Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.06-03-2010
20110207702BORON-CONTAINING SMALL MOLECULES AS ANTI-PROTOZOAL AGENTS - This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.08-25-2011
20090264384INDOLE, BENZIMIDAZOLE, AND BENZOLACTAM BORONIC ACID COMPOUNDS, ANALOGS THEREOF AND METHODS OF USE THEREOF - Benzimidazole, indole and benzolactam boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof.10-22-2009
20100137250NAPHTHYLACETIC ACIDS - The invention is concerned with the compounds of formula I:06-03-2010
20100137248BORON-CONTAINING COMPOUNDS, USES AND PREPARATION THEREOF - There are provided compounds of formulas (I) to (XIV) and compositions comprising such compounds. Such compounds and compositions are particularly useful for treating inflammation and/or pain, or for water treatment.06-03-2010
20110207701BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS - This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.08-25-2011
20080234228Boronic acid salts - Salts of a peptide boronic add drug, for example of Cbz-(R)-Phe-(S)-Pro-(R)-Mpg-B(OH)09-25-2008
20100004204ROS-SENSITIVE IRON CHELATORS AND METHODS OF USING THE SAME - The present invention provides compounds of Formula (I): along with compositions containing the same and methods of use thereof in treating oxidative stress.01-07-2010
20110230441STABLE BORTEZOMIB FORMULATIONS - Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base.09-22-2011
20110224171INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III).09-15-2011
20110230442NA CHANNELS, DISEASE, AND RELATED ASSAYS AND COMPOSITIONS - Disclosed are molecules and their synthesis, for use in blocking gated ion channels such as voltage-gated sodium channels (VGSCs) and prostate voltage sodium channels (PVSCs). These inhibitors have superior blocking efficacy, for instance in displacing the radioligand [09-22-2011
20110230440INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III).09-22-2011
20090099132Proteasome inhibitors - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.04-16-2009
20120077778Ladder-Frame Polyether Conjugates - Disclosed are compounds that are conjugates of ladder frame polyether compounds and biologically active compounds or research compounds, pharmaceutical formulations comprising the conjugates, and methods of transporting the conjugates across biological membranes.03-29-2012
20090209491Lactams as conformationally constrained peptidomimetic inhibitors - The present invention relates to inhibitors of post-proline cleaving enzyme, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention incorporate a lactam ring in the backbone of the inhibitors. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the target protease.08-20-2009
20090239824HYDROLYTICALLY-RESISTANT BORON-CONTAINING THERAPEUTICS AND METHODS OF USE - Compositions and methods of use of borole derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.09-24-2009
20090253653ANALOGS OF BENZOQUINONE-CONTAINING ANSAMYCINS AND METHODS OF USE THEREOF - The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting 17-ammonium hydroquinone ansamycin analog.10-08-2009
20100168062Quinoxaline Derivatives as Tyrosine Kinase Activity Inhibitors - The present invention relates to quinoxaline compound of the formula (I):07-01-2010
20100160257USE OF HDAC INHIBITORS FOR THE TREATMENT OF MYELOMA - The present invention relates to the use of an HDAC inhibitor, especially an HDAC inhibitor of formula (I)06-24-2010
20110130363BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.06-02-2011
20100261674THERAPEUTIC APPLICATIONS OF FATTY ACID AMIDE HYDROLASE INHIBITORS - Fatty acid amide hydrolase (FAAH) is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors). Disclosed herein are potent inhibitors of FAAH and methods for their use for treating a variety of disorder, including hypertension and cardiac hypertrophy.10-14-2010
20100240611METHODS FOR PREPARING DPP-IV INHIBITOR COMPOUNDS - Methods for preparing an inhibitor of dipeptidyl peptidase IV, as well as formulations of such inhibitors of dipeptidyl peptidase IV that have a high degree of stability including under warm, humid storage conditions.09-23-2010
20100152136TP53 Gene expression and uses thereof - The present invention is drawn to diagnosis, prognosis and treatment of multiple myeloma. In this regard, the present invention discloses importance of down-regulation of TP3 gene in multiple myeloma and its use as an independent progostic indicator of multiple myeloma. Additionally, the present invention also discloses novel-TP53 associated genes and demonstrates the clinical relevance of these alterations to disease progression.06-17-2010
20090075936Proteasome inhibitors and methods of using the same - The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly or indirectly with proteasome activity.03-19-2009
20100210593Pyridine- and Pyrimidinecarboxamides as CXCR2 Modulators - There is disclosed pyridine- and pyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include pyridine- and pyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.08-19-2010
20100113393Boronic Acid Salts - Salts of a peptide boronic acid drug, for example of Cbz-(R)-Phe-(S)-Pro-(R)-Mpg-B(OH)05-06-2010
20120142634Method of Treating Cancer with a Combination of a Proteasome Inhibitor and Salubrinal - The disclosure provides methods for treating or preventing a cancerous condition, such as multiple myeloma, by administering a therapeutically effective combination of a proteasome inhibitor and salubrinal.06-07-2012
20100197634INHIBITORS OF JANUS KINASES - The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.08-05-2010
20090209492Lipase Inhibitors - The present invention relates to inhibitors of lipases, such as inhibitors of endothelial lipase, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. The prototype of these inhibitors has lipophilic portion and an electrophilic site.08-20-2009
20120270840Proteasome inhibitors and processes for their preparation, purification and use - The invention provides boronic esters of Formula I10-25-2012
20110021462SUBSTITUTED TETRAHYDRO-2H-ISOQUINOLIN-1-ONE DERIVATIVES, AND METHODS FOR THE PRODUCTION AND USE THEREOF - This invention relates to compounds according to the general formula (I), where the definitions of the substituents R1, R2, Ar and X are as specified in the description, and to their physiologically tolerated salts, methods for the preparation of these compounds and their use as medicaments.01-27-2011
20110245203DERIVATIVES OF 1-AMINO-2-CYCLOPROPYLETHYLBORONIC ACID - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.10-06-2011
20100286092BETA-LACTAMASE INHIBITORS - Disclosed herein are α-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising α-aminoboronic acids and methods of use thereof.11-11-2010
20110086818METHODS, COMPOSITIONS, AND KITS FOR TREATING PAIN AND PRURITUS - The invention features methods, compositions, and kits for selective inhibition of pain-and itch sensing neurons (nociceptors and pruriceptors) by drug molecules of small molecule weight, while minimizing effects on non-pain-sensing neurons or other types of cells.04-14-2011
20090099131INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III).04-16-2009
20100056479THE USE OF QUATERNARY AMMONIUM COMPOUNDS IN THE REMEDIATION OF MOLD, MILDEW, AND FUNGUSES - The present invention relates to the use of quaternary ammonium compounds in the remediation of microbial growth such as mold, funguses, and mildew.03-04-2010
20100056478Useful Combinations of Monobactam Antibiotics With Beta-Lactamase Inhibitors - A pharmaceutically composition, comprising a combination of an antibiotically active compound of the formula (I): with a β-lactamase inhibitor of one of the formulae (II) to (XIII) are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another β-lactamase inhibitor of one of the formulae (II) to (XIII), particularly of formula (V) or formula (VI).03-04-2010
20110178040METHOD FOR TREATING FIBROSIS AND CANCER WITH IMIDAZOLIUM AND IMIDAZOLINIUM COMPOUNDS - There is presently provided methods for delivering an anti-fibrotic or anti-cancer agent to a cell. The methods comprise contacting a cell with an effective amount of imidazolium and imidazolinium compounds as described herein, including imidazolium and imidazolinium salts.07-21-2011
20110098248MODULATORS OF TOLL-LIKE RECEPTORS - The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.04-28-2011
20110082108Peptidomimetic Inhibitors of Post-Proline Cleaving Enzymes - The present invention relates to inhibitors of post-proline cleavage enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of side chains in the P1 and/or P2 position of the inhibitor. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.04-07-2011
20110152217POLYMORPHS OF (S)-3-AMINOMETHYL-7-(3-HYDROXY-PROPOXY)-3H-BENZO[C][1,2]OXABOROL-1-OL - This invention provides, among other things, polymorphs of the hydrochloride salt of (S)-3-aminomethyl-7-(3-hydroxy-propoxy)-3H-benzo[c][1,2]oxaborol-1-ol.06-23-2011
20110071112Compositions and Methods for Preserving Colors and Patterns of Plants - The present invention relates to a composition for preserving plants, which comprises 5 carbon alcohol, at least one alcohol selected from the group consisting of 3 carbon alcohol and 4 carbon alcohol, a thiourea and at least one acid selected from the group consisting of tartaric acid and boric acid. The composition is used to preserve colors, patterns and DNA of plants. The composition can also be used to change colors of flowers. The present invention also relates to a method for preserving plants, which comprises soaking the plants in the composition of the present invention.03-24-2011
20120035132BORON-CONTAINING SMALL MOLECULES - Compounds, pharmaceutical formulations, and methods of treating anti-inflammatory conditions and/or helminth-associated diseases are disclosed.02-09-2012
20120202775SUBSTITUTED INDOLE AND AZAINDOLE OXOACETYL PIPERAZINAMIDE DERIVATIVES - Compounds having drug and bio-affecting properties are described herein, including their properties, pharmaceutical compositions and methods of use. In particular, tricyclic aryl or heteroaryl piperazine diamide derivatives that possess unique antiviral activity are set forth. These compounds are useful for the treatment of HIV and AIDS. The compounds herein have the general Formula I:08-09-2012
20100305067ANTIBACTERIAL CONDENSED THIAZOLES - Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C12-02-2010
20110212919PROTEIN CROSS-LINKING INHIBITOR - The present invention provides a protein cross-linking inhibitor containing a compound represented by any of the following formulas (09-01-2011
20110212918BORON-CONTAINING SMALL MOLECULES - This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections.09-01-2011
20100056480USE OF ARGINASE INHIBITORS IN THE TREATMENT OF ASTHMA AND ALLERGIC RHINITIS - The present invention relates to the use of an arginase inhibitor for the preparation of a medicament for the prophylactic maintenance therapy of an asthmatic or allergic patient by preventing obstruction of upper and lower airways, in particular allergen-induced bronchial obstruction and/or airway hyperresponsiveness. The patients are either asthmatic or have allergic rhinitis. Preferably, the arginase inhibitor is 2(S)-amino-6-boronohexanoic acid (ABH).03-04-2010
20090082309Method of Regulating Glucose Metabolism, and Reagents Related Thereto - The present invention provides methods and compositions for modification and regulation of glucose and lipid metabolism, generally to reduce insulin resistance, hyperglycemia, hyperinsulinemia, obesity, hyperlipidemia, hyperlipoprotein-emia (such as chylomicrons, VLDL and LDL), and to regulate body fat and more generally lipid stores, and, more generally, for the improvement of metabolism disorders, especially those associated with diabetes, obesity and/or atherosclerosis.03-26-2009
20090062235Inhibitors of Dipeptidylpeptidase IV - The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of sidechains in the P1 and/or P2 position of the inhibitor that contain a carboxylic acid moiety. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.03-05-2009
20110178041HETEROCYCLIC BIARYL DERIVATIVE AND PDE INHIBITOR COMPRISING SAME AS ACTIVE INGREDIENT - Novel heterocyclic biaryl derivatives were disclosed which are useful as pharmaceutical agents and which exhibit a phosphodiesterase-inhibitory action.07-21-2011
20080287394Hiv Integrase Inhibitors - Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R11-20-2008
20120077779Inhibitors of Fibroblast Activation Protein Alpha - Disclosed are peptide-based compounds that include boronic acid or cyano functionality, which efficiently and selectively inhibit fibroblast activation protein alpha. Among other therapeutic utilities, the peptide-based compounds may be useful for the treatment of cancer.03-29-2012
20100323988SOLID CITRATE AND TARTRATE SALTS OF DPP-IV INHIBITORS - This invention relates to DPP-IV inhibitory citrate or tartrate salts of pyrrolidinylaminoacetyl pyrrolid acid compounds that are physically and chemically stable, substantially non-deliquescent solids under ambient conditions.12-23-2010
20110136763TRISUBSTITUTED BORON-CONTAINING MOLECULES - This invention largely relates to 3,4,6-trisubstituted benzoxaborole compounds, and their use for treating bacterial infections.06-09-2011
20100190748BORON-CONTAINING SMALL MOLECULES - This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.07-29-2010
20090176739OPTICAL ISOMERS OF AN ILOPERIDONE METABOLITE - The present invention relates to novel isomers of a metabolite of Iloperidone, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.07-09-2009
20100190749Benzoxazole kinase inhibitors and methods of use - The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications.07-29-2010
20110190235BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS - This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.08-04-2011
20090291917Boron-Containing Small Molecules as Anti-Inflammatory Agents - Compounds and methods of treating anti-inflammatory conditions are disclosed.11-26-2009
20090131367Combinations of HDAC Inhibitors and Proteasome Inhibitors - Provided herein are pharmaceutical agents, pharmaceutical compositions, methods of treatment, treatment regimens and kits for the treatment of cancer.05-21-2009
20100190750GPR119 Receptor Agonists in Methods of Increasing Bone Mass and of Treating Osteoporosis and Other Conditions Characterized by Low Bone Mass, and Combination Therapy Relating Thereto - The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. The present invention further relates to the use of a GPR119 receptor agonist in combination with a dipeptidyl peptidase IV (DPP-IV) inhibitor for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. A GPR119 receptor agonist and the combination of a GPR119 receptor agonist and a DPP-IV inhibitor promote bone formation in an individual.07-29-2010
20100009934BETA ADRENERGIC RECEPTOR AGONISTS FOR THE TREATMENT OF B-CELL PROLIFERATIVE DISORDERS - The invention features a method of treating a B-cell proliferative disorder by administering to a patient a BAR agonist, e.g., formulated for administration by a route other than inhalation (such as for oral or intravenous administration), in an amount effective to treat the B-cell proliferative disorder. The BAR agonist may be administered as a monotherapy or in combination with one or more other agents, e.g., a PDE inhibitor, an A2A receptor agonist, or an antiproliferative compound, in amounts that together are effective to treat the B-cell proliferative disorder. The invention further features pharmaceutical compositions and kits including a BAR agonist, alone or in combination with additional agents, for the treatment of a B-cell proliferative disorder.01-14-2010
20100249065Biomarkers for Assessing Peripheral Neuropathy Response to Cancer Treatment - The present invention provides methods for identifying patients at increased risk of developing an adverse neurological event in response to a cancer treatment. Methods also include modifying the treatment regimen of said patent dependent on the presence or absence of biomarkers in the patient.09-30-2010
20110118208Thiazolyl-Dihydro-Indazoles - The present invention encompasses compounds of general formula (1)05-19-2011
20090042837LEPTOMYCIN COMPOUNDS - Leptomycin-type compounds according to formula I02-12-2009
20110003771Wood Preservative Composition - A wood preservative composition comprising a mixture of a fungicide which is a combination of a boric acid ester, which is soluble in an organic solvent and has a sterically hindered di-alcohol or tri-alcohol group, such as trihexylene glycol biborate, an organo-iodine compound, a triazole, and a synthetic pyrethroid insecticide, said fungicide and the insecticide being present in a sufficient amount that wood treated with the wood treatment material contains fungicide and insecticide in an amount of about 1 ppm to 5000 ppm, based on the weight of the wood after treatment.01-06-2011
201200409339-(PIPERAZINYLALKYL) CARBAZOLES AS BAX-MODULATORS - piperazine compounds for use as pharmaceutically active compounds and in pharmaceutical formulations that are useful for the treatment of disorders associated with apoptosis, including neurodegenerative disorders, diseases associated with polyglutamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders, renal hypoxia, hepatitis and AIDS, where the piperazine compounds are represented by formula (I) and the terms R02-16-2012
20120040932CYCLIC BORONIC ACID ESTER DERIVATIVES AND THERAPEUTIC USES THEREOF - Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to 1 cyclic boronic acid ester derivatives and their use as therapeutic agents.02-16-2012
20100004205PHARMACEUTICAL COMPOSITIONS - Synergistic combinations of a squalene epoxidase inhibitor and a leucyl-tRNA synthetase inhibitor are provided, which are useful in particular in the treatment of diseases involving fungal or suspected fungal infection, for immunomodulation or immunosuppression in conditions in which fungal or suspected fungal colonisation of e.g. the skin or nail plays a role, such as atopic dermatitis, acne vulgaris, seborrhoeic dermatitis, rosacea or onychomycosis, and in situations of fungal resistance.01-07-2010
20110319360Method of including apoptosis/Cell death in leukemia cell using a purine nucleoside analogue - A method of inducing apoptosis or cell death in a leukemia cell includes subjecting the cell to a purine nucleotide analogue, LMP-420 (2-amino-6-chloro-9-[5(dihydroxyboryl)-pentyl] purine).12-29-2011
20120046243Aminopyridine- and Aminopyrimidinecarboxamides as CXCR2 Modulators - There is disclosed aminopyridine-and aminopyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include aminopyridine- and aminopyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.02-23-2012
20120004197PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR ANEMIA COMPRISING TETRAHYDROQUINOLINE COMPOUND AS ACTIVE INGREDIENT - Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin. Specifically disclosed is and EPO production enhancer and/or a hemoglobin production enhancer comprising a 1-acyl-4-(substituted oxy, substituted amino, or substituted thio)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by general formula (1) [wherein R01-05-2012
20110166104BORON-CONTAINING SMALL MOLECULES - This invention provides, among other things, novel compounds useful for treating inflammatory conditions, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.07-07-2011
20110166103BORON-CONTAINING SMALL MOLECULES - This invention provides, among other things, novel compounds useful for treating inflammatory conditions, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.07-07-2011
20120015906USES OF BORTEZOMIB IN PREDICTING SURVIVAL IN MULTIPLE MYELOMA PATIENTS - The present invention provides a method of predicting outcome of treatment for multiple myeloma based on determining certain cytogenetic anomalies and considering gene expression profiling risks. Also provided are statistical methods employed to define variables independently impacting outcomes. Further provided is method of treatment of myeloma patients.01-19-2012
20120065165COMPOSITIONS AND METHODS OF TREATING ENDOTHELIAL DISORDERS - Compositions and methods of treating endothelial disorders, including: asthma, erectile dysfunction, pulmonary hypertension, cardiovascular disorders, and other disorders, using a synergistic combination of at least one arginase inhibitor and at least one phosphodiesterase (PDE1), (PDE2) and/or (PDE5) inhibitor are described.03-15-2012
20120071445Combination Therapy for the Treatment of Multiple Myeloma - The present invention provides a method for treating multiple myeloma in a subject, comprising the step of administering to the subject a combination of COMPOUND 1 and bortezomib. The invention further provides a method for treating multiple myeloma in a subject, comprising the step of administering to the subject a combination of COMPOUND 1 and melphalan.03-22-2012
20110071113Thiazole Derivatives and Use Thereof - The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.03-24-2011
20110082109NOVEL ACYL GUANIDINE DERIVATIVES - The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na04-07-2011
20090093443COMBINATIONS OF 4- BROMO-2-(4-CHLOROPHENYL)-5-(TRIFLUOROMETHYL)-1H-PYRROLE-3-CARBONITRILE AND BIOCIDAL COMPOUNDS - The present invention relates to combinations of 4-bromo-2-(4-chloro-phenyl)-5-(trifluoromethyl)-1H-pyrrole-3-carbonitrile, or a salt thereof, and a biocidal compound which provide an improved protecting effect against fouling organisms. More particularly, the present invention relates to compositions comprising a combination of 4-bromo-2-(4-chlorophenyl)-5-(trifluoromethyl)-1H-pyrrole-3-carbonitrile, or a salt thereof, together with one or more biocidal compounds selected from (4-isopropyl-pyridinio)methyldiphenylboron, triphenylboron pyridine, benzalkonium chloride, capsaicine, clonidine, fenazaquin, glutaric dialdehyde, menadione sodium bisulfite, menadione piperazine bisulfite, menadione triaminetriazine bisulfite, menthol or a derivative thereof, N,N-bis(3-aminopropyl)dodecylamine, coco(fractionated)benzyldimethylammonium chloride, peracetic acid, pyridaben, tebufenpyrad, and zosteric acid; in respective proportions to provide a synergistic effect against fouling organisms and the use of these compositions for protecting materials against fouling organisms.04-09-2009
20110105432AMINOCARBOXYLIC ACID DERIVATIVE AND MEDICINAL USE THEREOF - The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like.05-05-2011
20110105431Boronic Acid Aryl Analogs - The present invention relates to novel boronic acid aryl derivatives which are useful as antitumor/anticancer agents. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good inhibitors of the growth of human breast cancer cells. The present invention also relates to the use of the novel boronic acid aryl derivatives to treat cancer. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of cancer.05-05-2011
20090131366Use of Amine-Borane Compounds as Anti-Microbial Agents - Use of amine-borane compounds such as amine cyanoboranes and amino carboxy boranes in the treatment of medical conditions associated with pathogenic microorganisms and particularly against drug-resistant microorganisms, in the treatment of fungal and protozoal infections is disclosed. Use of amine-borane compounds for reducing the load of microorganisms in various substrates and products is further disclosed.05-21-2009
20110112051Dipeptidyl Peptidase-IV Inhibitors - The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.05-12-2011
20120264714BORON-CONTAINING SMALL MOLECULES AS ANTI-INFLAMMATORY AGENTS - Methods of treating anti-inflammatory conditions through the use of boron-containing small molecules are disclosed.10-18-2012
20120129807METHODS OF TREATMENT, IMPROVEMENT AND PREVENTION USING HALOARYL SUBSTITUTED AMINOPURINES - Provided herein are Aminopurine Compounds having the following structure:05-24-2012
20120129806ARGINASE INHIBITORS AS THERAPEUTICS - Compounds according to Formula I are potent inhibitors of Arginase I and II activity:05-24-2012
20120258933COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering a proteasome inhibiting compound, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, and optional additional antineoplastic agents, to a human in need thereof.10-11-2012
20120214765BORON-CONTAINING SMALL MOLECULES AS ANTI-INFLAMMATORY AGENTS - Compounds and methods of treating anti-inflammatory conditions are disclosed.08-23-2012
20120135959Metalloprotein inhibitors containing nitrogen based ligands - Provided herein metalloproteinase inhibitors containing nitrogen or mixed nitrogen/oxygen donating zinc binding groups. Also provided are pharmaceutical compositions containing the compounds and methods of treating preventing or ameliorating the diseases associated with metalloproteinase activity using the compounds and compositions.05-31-2012
20120172335SUBSTITUTED BENZIMIDAZOLONE DERIVATIVES, MEDICAMENTS COMPRISING THEM AND THEIR USE - The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R07-05-2012
20100222301TOPICAL DRUG FOR TREATMENT AND/OR PREVENTION OF DIABETIC NEUROPATHY, MICROANGIOPATHY AND DIABETIC AND NON DIABETIC ULCERS AND WOUND INFECTION - The various embodiments herein provide a topical drug composition for the treatment of diabetes-related complications. According to one embodiment herein, the composition comprises of a compound belonging to a group of chemicals containing borates. Boric acid is used as the base material of the drug. Boric acid is dissolved in saline 0.9% or half saline serum or water, distilled water or boiled water to obtain a boric acid solution with given concentration. The best concentration is 3-5% solution. Alcohol at preset concentration is added to the boric acid solution. According to another embodiment, a method is provided for preparing a topical drug composition for the treatment of diabetes-related disorders.09-02-2010
20100286090Treatment of Multiple Myeloma - Methods for treating multiple myeloma comprising administering a therapeutically effective amount of dasatinib to a patient in need of treatment thereof. Dasatinib can be administered alone or in combination with a second anti-neoplastic agent such as dexamethasone or bortezomib. The patient may be refractory to prior treatment with an anti-neoplastic agent other than dasatinib.11-11-2010
20100292185BETA-LACTAMASE INHIBITORS - Disclosed herein are α-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising α-aminoboronic acids and methods of use thereof.11-18-2010
20120083469INHIBITORS OF ARGINASE AND THEIR THERAPEUTIC APPLICATIONS - Compounds according to Formula I and Formula II are potent inhibitors of Arginase I and II activity:04-05-2012
20110124597BORON CONTAINING SMALL MOLECULES - This invention provides, among other things, novel compounds useful for treating bacterial infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.05-26-2011
20100204180PROTEASOME INHIBITORS - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.08-12-2010
20120322762Stable Bortezomib Formulations - Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base.12-20-2012
20110212920N-Substituted Benzene Sulfonamides - Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease.09-01-2011
20120322763Stable Bortezomib Formulations - Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base.12-20-2012
20120101062Lipase Inhibitors - The present invention relates to inhibitors of lipases, such as inhibitors of endothelial lipase, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. The prototype of these inhibitors has lipophilic portion and an electrophilic site.04-26-2012
20120149663BORONIC ACID COMPOSITIONS AND METHODS RELATED TO CANCER - Disclosed are compounds and methods related to boronic acid derivatives of resveratrol. Certain of these derivatives have enhanced efficacy relative to resveratrol, function as irreversible modulators, and act at the GI/S phase of the cell cycle.06-14-2012
20110160160METHODS FOR HEAT SHOCK PROTEIN DEPENDENT CANCER TREATMENT - The present invention provides a method of treating an Hsp70 dependent cancer, including: providing at least one Hsp70 dependent cancer cell; contacting the at least one cell with a sub-effective concentration of a dihydropyrimidinone compound; and contacting the at least one cell with a sub-effective concentration of a proteasome inhibitor, wherein the sub-effective concentration of the dihydropyrimidinone compound and the sub-effective concentration of the proteasome inhibitor have a synergistic effect upon the at least one cell.06-30-2011
20130023494MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO - The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an SGLT2 inhibitor, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.01-24-2013
20080234229Novel Therapeutic Agents for the Treatment of Cancer, Metabolic Diseases and Skin Disorders - The present invention is directed to compounds having the structure Formula (I) wherein R09-25-2008
20080221069Novel Therapeutic Agents for the Treatment of Cancer, Metabolic Diseases and Skin Disorders - The present invention is directed to novel compounds according to formula (I) wherein R09-11-2008
20080221067Wood preservative composition - A wood preservative composition comprising a mixture of a fungicide which is a combination of a boric acid ester, which is soluble in an organic solvent and has a sterically hindered di-alcohol or tri-alcohol group, such as trihexylene glycol biborate, an organo-iodine compound, a triazole, and a synthetic pyrethroid insecticide, said fungicide and the insecticide being present in a sufficient amount that wood treated with the wood treatment material contains fungicide and insecticide in an amount of about 1 ppm to 5000 ppm, based on the weight of the wood after treatment.09-11-2008
20080214501BRUTON'S TYROSINE KINASE ACTIVITY PROBE AND METHOD OF USING - Described herein are probes for Bruton's tyrosine kinase (Btk). Such probes are used to characterize and develop Btk-selective inhibitors intended for therapeutic use.09-04-2008
20130096086MITOCHONDRIA AND HUMAN IMMUNODEFIENCY VIRUS TYPE 1 - Methods described herein relate to mitochondria and their role in Human immunodeficiency virus type 1 (HIV-1) infection and cell-to-cell HIV-1 transmission and compositions and methods for modulating mitochondrial mediated cell-to-cell transmission of HIV-1. Methods for screening to identify inhibitors of mitochondrial mediated cell-to-cell transmission of HIV-1 are also envisioned herein.04-18-2013
20130096085PROCHELATORS USEFUL FOR INHIBITING METAL-ASSOCIATED TOXICITY - Prochelator compounds of Formula (I) or Formula (II) are described, along with methods of using the same and pharmaceutical formulations or compositions containing the same.04-18-2013
20130131016BORON-CONTAINING SMALL MOLECULES - This invention provides novel compounds, methods of using the compounds, and pharmaceutical formulations comprising the compounds.05-23-2013
20130131017BORON-CONTAINING SMALL MOLECULES - This invention provides novel compounds, methods of using the compounds, and pharmaceutical compositions containing the compounds.05-23-2013
20080200434Chemical Target-Binding Compositions - Herein is described compositions and methods for modulating and regulating the concentration of a chemical target in an organism or in an ecosystem. In one embodiment, the concentration is regulated such that it is maintained below or above a certain threshold, thus avoiding toxic or harmful effects of the chemical target. The described compositions may, for example, be implanted in a human body or placed in the ecosystem. The compositions comprise binding moieties that reversibly bind to a chemical target in the organism or ecosystem. The binding capacity and the binding constants for a chemical target are designed such that the composition maintains the concentration of the chemical target substantially within a beneficial range of concentrations.08-21-2008
20080200433Molecular Chaperone Function Regulator - According to the present invention, a molecular chaperone function regulator containing a quinazoline derivative represented by the following formula (I)08-21-2008
20110275597PHARMACEUTICAL COMPOSITION - The present invention relates to a parenteral pharmaceutical composition comprising therapeutically effective amounts of N-(2-pyrazine)carbonyl-L-phenylalanine-L-leucine boronic acid or its salts or its derivatives and tromethamine wherein the composition is stable.11-10-2011
20110275596METHODS FOR TREATING NEOPLASIA AND FOR IDENTIFYING COMPOSITIONS USEFUL IN SUCH THERAPY - Various methods for treating a patient with neoplasia are disclosed, in particular, methods using topoisomerase Ila-preferential poisons, methods using a combination of a topoisomerase Illi-preferential inhibitor and a topoisomerase II poison, and methods using a combination of a topoisomerase II poison and a proteasome inhibitor are disclosed. Novel topoisomerase Ila-preferential poisons are disclosed, particularly, several novel 13-carboline derivatives are identified. Methods for identifying the novel topoisomerase Ila-preferential poisons and methods for identifying the novel topoisomerase EP-preferential inhibitors are also provided herein.11-10-2011
20110237547PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF FUNGAL INFECTIONS - Synergistic combinations of a squalene epoxidase inhibitor and a leucyl-tRNA synthetase inhibitor are provided, which are useful in particular in the treatment of diseases involving fungal or suspected fungal infection, for immunomodulation or immunosuppression in conditions in which fungal or suspected fungal colonisation of e.g. the skin or nail plays a role, such as atopic dermatitis, acne vulgaris, seborrhoeic dermatitis, rosacea or onychomycosis, and in situations of fungal resistance.09-29-2011
20130150326AUTOTAXIN INHIBITORS AND USES THEREOF - Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.06-13-2013
20100286091IMIDAZOLIDINONE COMPOUNDS, METHODS TO INHIBIT DEUBIQUITINATION AND METHODS OF TREATMENT - The present invention features imidazolidinone compounds and pharmaceutical compositions of imidazolidinone compounds. The compounds of the invention are utilized in methods of treating a deubiquitination-related disorder in a subject and inhibiting p97-associated deubiquitination.11-11-2010
20100317621BETA-LACTAMASE INHIBITORS - Disclosed herein are α-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising α-aminoboronic acids and methods of use thereof.12-16-2010
20130157977Benzimidazole Boronic Acid Derivatives As PI3 Kinase Inhibitors - This invention relates to the use of benzimidazole boronic acid derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazole boronic acids in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazole boronic acid compounds for treating cancer.06-20-2013
20130190273Methods for Treating Amyotrophic Lateral Sclerosis Using Pro-Neurogenic Compounds - This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.07-25-2013
20110319361BORON-CONTAINING SMALL MOLECULES - This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.12-29-2011
20090312284HISTONE DEACETYLASE INHIBITORS WITH COMBINED ACTIVITY ON CLASS-I AND CLASS-IIB HISTONE DEACETYLASES IN COMBINATION WITH PROTEASOME INHIBITORS - The present invention is concerned with combinations of a proteasome inhibitor and a histone deacetylase inhibitor with combined activity on class-I and class-IIb histone deacetylases, for inhibiting the growth of tumor cells, useful in the treatment of cancer.12-17-2009
20120088738INHIBITORS OF FATTY ACID AMIDE HYDROLASE - Provided herein are compounds of formula (I): or pharmaceutically acceptable salts, solvates or prodrugs thereof or mixtures thereof, wherein Z04-12-2012
20120094957INHIBITORS OF FATTY ACID AMIDE HYDROLASE - Provided herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof, or mixtures thereof, wherein Z04-19-2012
20130210770PHARMACEUTICAL FORMULATIONS - This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.08-15-2013

Patent applications in class Boron containing DOAI